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Assay Detail

CHEMBL5364540

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Bronchoconstriction activity in Sprague-Dawley rat trachea assessed as inhibition of carbachol-induced tracheal contraction
10
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Trachea
Confidence 1 — Organism
Curated By Autocuration

Target

Trachea (CHEMBL4296542)
Type TISSUE
Organism Rattus norvegicus

Publication

Optimization of M<sub>3</sub> Antagonist-PDE4 Inhibitor (MAPI) Dual Pharmacology Molecules for the Treatment of COPD.
Rizzi A, Amari G, Pivetti F, Delcanale M, Amadei F, Pappani A, Fornasari L, Villetti G, Marchini G, Pisano AR, Pitozzi V, Pittelli MG, Trevisani M, Salvadori M, Cenacchi V, Fioni A, Puccini P, Civelli M, Patacchini R, Baker-Glenn C, Van de Poël H, Blackaby W, Nash K, Armani E.
J Med Chem (2023) 66 : 11476 -11497
PubMed 37561958 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 8.06 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5426968 1 9.00
CHEMBL5395712 2 8.60
CHEMBL5408238 2 8.40
CHEMBL5409010 1 8.40
CHEMBL5417689 1 7.90
CHEMBL5399363 2 7.80
CHEMBL5410533 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5426968 IC50 = 1.0 nM 9.00
CHEMBL5395712 IC50 = 2.512 nM 8.60
CHEMBL5395712 IC50 = 3.162 nM 8.50
CHEMBL5408238 IC50 = 3.981 nM 8.40
CHEMBL5409010 IC50 = 3.981 nM 8.40
CHEMBL5417689 IC50 = 12.59 nM 7.90
CHEMBL5399363 IC50 = 15.85 nM 7.80
CHEMBL5410533 IC50 = 25.12 nM 7.60
CHEMBL5408238 IC50 = 39.81 nM 7.40
CHEMBL5399363 IC50 = 100.0 nM 7.00